Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SY-5609 is a selective and noncovalent inhibitor of CDK7(KD = 0.065 nM) with antitumor activity and inhibits apoptosis.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
---|---|---|---|---|---|
サンプルについてお問い合わせ | |||||
1 mg | 在庫あり | ¥ 32,500 | |||
2 mg | 在庫あり | ¥ 48,500 | |||
5 mg | 在庫あり | ¥ 83,000 | |||
10 mg | 在庫あり | ¥ 134,000 | |||
25 mg | 在庫あり | お問い合わせ | |||
50 mg | 在庫あり | お問い合わせ | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 96,500 |
説明 | SY-5609 is a selective and noncovalent inhibitor of CDK7(KD = 0.065 nM) with antitumor activity and inhibits apoptosis. |
ターゲット&IC50 | CDK12:870 nM (Ki), CDK7:0.065 nM (Kd), CDK9:960 nM (Ki), CDK2:2600 nM (Ki) |
In vitro | SY-5609 (126.4 pM-4 µM) has an EC50 of 5.6 nM in the HCC70 cell line[1]. SY-5609 (0.01-10000 nM) exhibits strong antiproliferative effects with IC50s of 1-6 nM in triple-negative breast cancer and ovarian cancer cells including HCC70, MDA-MB453, COV504, A2780, OVCAR3, CAOV3 cells. SY-5609 (100-500 nM) induces apoptosis in HCC70, MDA-MB-468, CAOV3, and OVCAR3 cells. In HCC70 cells, SY-5609 (100-500 nM) induces G2/M cell cycle arrest. SY-5609 (25-500 nM) inhibits the phosphorylation of CDK2 at Thr160 via loss of CAK function[2]. |
In vivo | In Balb/c nude female mice with HCC70 cell lines, SY-5609 (2 mg/kg/day; orally) induces tumor regression with a plasma exposure of 261.28 ng h/mL, a Cmax of 50.67 ng/mL and an elimination half-life of 3.33 h[2]. |
別名 | CDK7-IN-3 |
分子量 | 490.46 |
分子式 | C23H26F3N6OP |
CAS No. | 2417302-07-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 36 mg/mL (73.4 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
SY-5609 2417302-07-7 Cell Cycle/Checkpoint CDK SY5609 SY 5609 CDK7-IN-3 Inhibitor inhibitor inhibit